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    PREPARATION OF [2-METHYL-5-PHENYL-3-(PIPERAZIN-1-YLMETHYL)] PYRROLE DERIVATIVES
    11.
    发明申请
    PREPARATION OF [2-METHYL-5-PHENYL-3-(PIPERAZIN-1-YLMETHYL)] PYRROLE DERIVATIVES 审中-公开

    公开(公告)号：US20090118509A1

    公开(公告)日：2009-05-07

    申请号：US11911272

    申请日：2006-04-05

    Applicant: Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Om Dutt Tyagi ,  Vasanth Nalam ,  Yogendra Kumar Chauhan

    Inventor： Sudershan Kumar Arora ,  Neelima Sinha ,  Sanjay Jain ,  Ram Shankar Upadhayaya ,  Om Dutt Tyagi ,  Vasanth Nalam ,  Yogendra Kumar Chauhan

    IPC: C07D401/14

    CPC classification number: C07D207/50 ,  C07D207/335 ,  C07D401/04 ,  C07D401/12

    Abstract: A process for the preparation of compounds of Formula I and their pharmaceutically acceptable acid addition salt wherein, R1 is phenyl or substituted phenyl R2 is selected from a group consisting of phenyl which is unsubstituted or substituted with 1 or 2 substituents, each independently selected from Cl, F, or pyridine, or naphthalene, or NHCOR4 wherein R4 is aryl, unsubstituted or substituted heteroaryl, unsubstituted or substituted heterocyclyl. R3 is selected from a group of formula wherein R5 is phenyl which is unsubstituted or substituted with 1 or 2 substituents each independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, nitro, amino, haloalkyl, haloalkoxy etc.; unsubstituted or substituted benzyl; unsubstituted or substituted heteroaryl; unsubstituted or substituted heteroaroyl; unsubstituted or substituted diphenylmethyl, n=0-2 and X═—NCH3, CH2, S, SO, or SO2 Such that when R2 is phenyl, which is unsubstituted or substituted with 1 or 2 substituents, each independently selected from Cl, F; R5 is not C1-C4 alkyl, or X is not —NCH3, CH2, S, SO, or SO2, when n=1, or X is not —CH2 when n=0; comprising the steps of (a) reacting compound of Formula II with a chlorinating agent in the presence or absence of catalytic amount of N,N-dimethylformamide to yield the compound of Formula III, (b) reacting the compound of Formula III with a compound of Formula R1H (R1 is as defined above), in presence of a Lewis acid to obtain the compound of Formula IV, (c) reacting the compound of Formula IV with a compound of Formula R2NH2 (R2 is as defined above) in presence of catalytic amounts of an aryl or alkyl sulphonic acid in an organic solvent to obtain the compound of Formula V, (d) reacting the compound of Formula V with various secondary amines of the Formula R3H (R3 is as defined above) in the presence of formaldehyde and acetic acid in acetonitrile followed by crystallization yield the compound of Formula I, (e) purifying the compound of Formula I by crystallization, (f) converting the purified compound of Formula I to a pharmaceutically acceptable acid addition salt.

    Antimycobacterial compounds
    15.
    发明授权
    Antimycobacterial compounds 失效
    抗分解细菌化合物

    公开(公告)号：US07691889B2

    公开(公告)日：2010-04-06

    申请号：US11082947

    申请日：2005-03-18

    Applicant: Sudershan Kumar Arora ,  Vijaykumar Jagdishwar Patil ,  Prathap Sreedharan Nair ,  Prasad Purushottam Dixit ,  Shankar Ajay ,  Rakesh Kumar Sinha

    Inventor： Sudershan Kumar Arora ,  Vijaykumar Jagdishwar Patil ,  Prathap Sreedharan Nair ,  Prasad Purushottam Dixit ,  Shankar Ajay ,  Rakesh Kumar Sinha

    IPC: A61K31/422 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/454 ,  A61K31/496 ,  C07D263/20 ,  C07D413/02 ,  C07D417/02

    CPC classification number: C07D263/20 ,  C07D413/10 ,  C07D413/14

    Abstract: Novel compounds belonging to the class of oxazolidinones possessing potent antimycobacterial properties especially useful in the treatment of acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai. The compound and its pharmaceutically acceptable salts act as antibacterial agents. Also mentioned is a method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial conditions such as Mycobacterium tuberculosis, drug resistant Mycobacterium tuberculosis, Mycobacterium avium-intracellular complex, M. fortuitum and M. kansai., including administering an antimycobacterially effective amount of the compound and/or pharmaceutically acceptable salts. There is also mentioned a process for the manufacture of the compound or its pharmaceutically acceptable salts.

    Abstract translation: 属于恶唑烷酮类的新型化合物具有强效的抗分支杆菌特性，特别适用于治疗结核分枝杆菌，鸟分枝杆菌 - 细胞内复合物，偶然遗传和关西等酸性快速生物。 该化合物及其药学上可接受的盐作为抗菌剂。 还提及了抑制分枝杆菌细胞生长的方法以及治疗结核分枝杆菌，耐药性结核分枝杆菌，鸟分枝杆菌 - 细胞内复合物，偶然和关西的分枝杆菌病症的方法，包括施用抗菌分泌杆菌 化合物和/或其药学上可接受的盐的量。 还提及了制备化合物或其药学上可接受的盐的方法。

    Substituted azabicyclo hexane derivatives as muscarinic receptor antagonists
    17.
    发明授权
    Substituted azabicyclo hexane derivatives as muscarinic receptor antagonists 失效
    取代的氮杂双环己烷衍生物作为毒蕈碱受体拮抗剂

    公开(公告)号：US07517905B2

    公开(公告)日：2009-04-14

    申请号：US10552456

    申请日：2003-04-09

    Applicant: Anita Mehta ,  Bruhaspathy Miriyala ,  Sudershan Kumar Arora ,  Jang Bahadur Gupta

    Inventor： Anita Mehta ,  Bruhaspathy Miriyala ,  Sudershan Kumar Arora ,  Jang Bahadur Gupta

    IPC: A61K31/403 ,  C07D209/52

    CPC classification number: C07D209/52

    Abstract: This invention relates to the derivatives of substituted azabicyclo hexanes. The compounds of this invention can function as muscarinic receptor antagonists and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.

    Abstract translation: 本发明涉及取代的氮杂双环己烷的衍生物。 本发明的化合物可用作毒蕈碱受体拮抗剂，可用于治疗通过毒蕈碱受体介导的呼吸，泌尿和胃肠系统的各种疾病。 本发明还涉及制备本发明化合物的方法，含有本发明化合物的药物组合物和通过毒蕈碱受体介导的疾病的治疗方法。

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